FTY720, an immune modulator, down-regulates sphingosine-1-phosphate (S1P) receptors, enhances the activity of sphingosine transporter Abcb1 and leukotriene C4 transporter Abcc1, and inhibits cytosolic phospholipase A2 activity. Its efficacy relies on in vivo phosphorylation by sphingosine kinases, resulting in FTY720-phosphate which also down-regulates S1P receptors. NBD-FTY720, a fluorescently-labeled analog of FTY720, retains the hydroxy methyl side chain targeted for phosphorylation, suggesting potential phosphorylation in vivo.
Diacylglycerols (DAG) are generated through the hydrolysis of membrane phospholipids and function as lipid second messengers by activating protein kinase C (PKC) and modulating cell growth and apoptosis. Additionally, they act as precursors for DAG kinases in the synthesis of phosphatidic acid, a crucial lipid messenger. The compound 1-NBD-decanoyl-2-decanoyl-sn-glycerol incorporates a nitrobenzoxadiazole (NBD) fluorophore at the ω-end of its terminal decanoyl chain, using the structure of 1,2-didecanoyl-sn-glycerol as a model for diacylglycerol. This molecule is expected to exhibit excitation and emission peaks at roughly 470/541 nm, paralleling those of various NBD-labeled phospholipids. Fluorescently labeled lipids, such as this, are instrumental in exploring their interactions with proteins, their uptake by cells and liposomes, and in developing assays for lipid metabolism research.
A cell-permeable synthetic peptide NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region is shown to block TNF-alpha-induced NF-kB activation. The interaction of IKγNEMO with the IKK complex is vital for t
22-NBD cholesterol, a fluorescent cholesterol analog featuring a nitrobenzoxadiazole (NBD) group, serves multiple research purposes in both in vitro and in vivo settings. Its applications span the analysis of steroid uptake and esterification, the study of intracellular localization and targeting, cholesterol metabolism in mammalian and bacterial cells, and examining cholesterol intestinal absorption in hamsters. This compound showcases excitation/emission maxima at 472/540 nm when integrated into 1,2-dimyristoyl-sn-glycero-3-PC (DMPC) vesicles. Notably, the emission maximum of 22-NBD cholesterol varies with the solvent's polarity, becoming more pronounced as the polarity increases.